Artemisinin and its derivatives (collectively termed as artemisinins) are among the most important and effective antimalarial drugs, with proven safety and efficacy in clinical use. Beyond their antimalarial effects, artemisinins have also been shown to possess selective anticancer properties, demonstrating cytotoxic effects against a wide range of cancer types both in vitro and in vivo. These effects appear to be mediated by artemisinin‐induced changes in multiple signaling pathways, interfering simultaneously with multiple hallmarks of cancer. Great strides have been taken to characterize these pathways and to reveal their anticancer mechanisms of action of artemisinin. Moreover, encouraging data have also been obtained from a limited number of clinical trials to support their anticancer property. However, there are several key gaps in knowledge that continue to serve as significant barriers to the repurposing of artemisinins as effective anticancer agents. This review focuses on important and emerging aspects of this field, highlighting breakthroughs in unresolved questions as well as novel techniques and approaches that have been taken in recent studies. We discuss the mechanism of artemisinin activation in cancer, novel and significant findings with regards to artemisinin target proteins and pathways, new understandings in artemisinin‐induced cell death mechanisms, as well as the practical issues of repurposing artemisinin. We believe these will be important topics in realizing the potential of artemisinin and its derivatives as safe and potent anticancer agents.

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青蒿素作为抗癌药物：靶点分析和作用机制的最新进展

青蒿素及其衍生物（统称为青蒿素）是最重要和最有效的抗疟药物之一，在临床使用中已证明其安全性和有效性。除了它们的抗疟作用外，青蒿素还被证明具有选择性抗癌特性，在体外和体内都显示出对多种癌症类型的细胞毒性作用。这些效应似乎是由青蒿素诱导的多种信号通路变化介导的，同时干扰多种癌症标志。已经在表征这些途径和揭示其青蒿素的抗癌作用机制方面取得了很大进展。此外，还从有限数量的临床试验中获得了令人鼓舞的数据，以支持其抗癌特性。然而，有几个关键的知识空白继续成为将青蒿素重新用作有效抗癌剂的重大障碍。本综述重点关注该领域的重要和新兴方面，重点介绍未解决问题的突破以及最近研究中采用的新技术和方法。我们讨论了青蒿素在癌症中的激活机制、关于青蒿素靶蛋白和途径的新发现和重要发现、对青蒿素诱导细胞死亡机制的新理解，以及重新利用青蒿素的实际问题。我们相信这些将是实现青蒿素及其衍生物作为安全有效抗癌剂潜力的重要课题。